Inhibition of Na+,K+-ATPase activity by (-)-ent-Kaur-16-en-19-oic acid and its derivatives

Planta Med. 2003 Jun;69(6):555-6. doi: 10.1055/s-2003-40636.

Abstract

The diterpene, (-)- ent-kaur-16-en-19-oic acid, from Croton oblongifolius was identified as an Na +,K +-ATPase inhibitor. This compound exhibits an IC 50 of 2.2 x 10( -5 )M against crude enzyme Na +,K +-ATPase from rat brain. The semi-synthetic derivatives, (-)-methyl kaur-16-en-19-oate, (-)-kaur-16-en-19-ol, (-)-16beta,17-epoxykauran-19-oic acid and (-)-17-hydroxykaur-15-en-19-oic acid were also tested and their IC 50 were 5.5 x 10 (-4), 5.0 x 10( -4), 4.8 x 10( -4) and 6.0 x 10 (-4) M, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / enzymology
  • Croton*
  • Diterpenes / administration & dosage
  • Diterpenes / pharmacology*
  • Diterpenes / therapeutic use
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Inhibitory Concentration 50
  • Phytotherapy*
  • Plant Bark
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use
  • Plant Stems
  • Rats
  • Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors*

Substances

  • Diterpenes
  • Enzyme Inhibitors
  • Plant Extracts
  • argyrophilic acid
  • Sodium-Potassium-Exchanging ATPase